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[摘要]：As a part of systematic investigation of synthesis and biologically active compounds of thiazolidine (TZD) derivatives containing pyrazole ring system, several new pyrazoleTZD derivatives 8a-d and 9a-d have been synthesized. Compounds 8a-d were prepared from N-substituted TZDs 6a-d and 1H-pyrazole-4-carboxaldehyde 7 by Knoevenagel-type reaction. Treatment of 8a-d with sodium hydride at room temperature caused dimerization reaction to afford the corresponding spirocompounds 9a-d. All the synthesized compounds were characterized by spectroscopic analysis. In vitro, the synthesized compounds 8a-d and 9a-d were tested for their growth inhibitory activity in A549 lung cancer, B16F10 murine melanoma, and HeLa human uterine carcinoma cells and for their differentiation of 3T3-L1 preadipocytes to adipocytes. The results showed that compound 8c possessed growth inhibitory effect of B16F10 cells (IC50 = 27 mu M) and compounds 9c,d had induction effect on the differentiation of 3T3-L1 preadipocytes. J. Heterocyclic Chem., (2011). |
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